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DOI: 10.1055/s-0036-1596364
In vitro antioxidant and anticancer properties of hydroethanolic extracts, fractions and novel flavones of Ageratum conyzoides leaves
Publication History
Publication Date:
14 December 2016 (online)
Ageratum conyzoides L (Asteraceae) has increasingly been used in folklore for the treatment of a wide range of diseases including cancer [1] This study was aimed at investigating the anticancer potential of 50% hydroethanolic leaf extracts, fractions and compounds isolated from Ageratum conyzoides against Jurkat cells using standard methods This study also reports the isolation of a novel flavone, 8-chloro-5-hydroxy-2-(4-hydroxy-3,5-dimethoxyphenyl)-7-methoxy-4 H-chromen-4-one Mean IC50 values were compared by one way ANOVA The 50% hydroethanolic leaf extract as well as the chloroform and ethylacetate fractions exhibited cytotoxicities against Jurkat cells with IC50 values of 151 ± 03 µg/ml, 636 ± 16 µg/ml and 46 ± 01 µg/ml, respectively compared to curcumin, 0002 ± 00 µg/ml and had strong selectivity indices (SI) against Jurkat cells with values of 6633, 1572 and 2174, respectively compared to curcumin (SI = 23) Treatments with purified flavones (5,6,7,3',4',5'-Hexamethoxyflavone, 5,6,7,8,3',4'-Hexamethoxyflavone and 5,6,7,3',4'-Pentamethoxyflavone) showed strong cytotoxic effect in a dose responsive manner Only 5,6,7,3',4',5'-Hexamethoxyflavone and 5,6,7,8,3',4'-Hexamethoxyflavone induced apoptosis through caspase 3/7 activation in a dose-dependent manner compared to staurosporine, positive control For the first time 5,6,7,3',4',5'-Hexamethoxyflavone and 5,6,7,8,3',4'-Hexamethoxyflavone have been shown to exert cytotoxic effects against Jurkat cells via induction of apoptosis Physicochemical properties such as albumin binding (% HSA), affinity to phosphatidylcholine (CHI IAM74 scores) and volume of distribution (Log Vd) predicted for these compounds assume that the cytotoxicity observed is due to on-target action and not off-target effects This suggests that these bioactive components found in A conyzoides could be useful in the development of new leukemic therapies
Keywords: Ageratum conyzoides, cytotoxicity, flavone, Jurkat.
References:
[1] Acheampong F, Larbie C, Appiah-Opong R, Arthur FKN, Tuffour I. In vitro antioxidant and anticancer properties of hydroethanolic extracts and fractions of Ageratum cornyzoides. EJMP 2015; 7: 204 – 215